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K-858

Cat. No. M7876
K-858 Structure
Synonym:

Racemic

Size Price Availability Quantity
5mg USD 48  USD48 In stock
10mg USD 88  USD88 In stock
50mg USD 320  USD320 In stock
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Quality Control & Documentation
Biological Activity

Eg5 is a key protein involved in the formation of bipolar spindles. K858 is a selective ATP-uncompetitive mitotic kinesin Eg5 inhibitor. The compound induces mitotic arrest, caspase-3 activation and cell growth inhibition in HCT116 cells.

Chemical Information
Molecular Weight 277.34
Formula C13H15N3O2S
CAS Number 72926-24-0
Solubility (25°C) DMSO ≥ 30 mg/mL
Storage Powder          -20°C   3 years ;  4°C   2 years
In solvent       -80°C   6 months ;  -20°C   1 month
Conversion of different model animals based on BSA (PMID: 27057123)
Species Mouse Rat Rabbit Guinea pig Hamster Dog
Weight (kg) 0.02 0.15 1.8 0.4 0.08 10
Body Surface Area (m2) 0.007 0.025 0.15 0.05 0.02 0.5
Km factor 3 6 12 8 5 20
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.

References

[1] Sandeep K Talapatra, et al. Crystal structure of the Eg5 - K858 complex and implications for structure-based design of thiadiazole-containing inhibitors

[2] Sabrina Giantulli, et al. Growth arrest and apoptosis induced by kinesin Eg5 inhibitor K858 and by its 1,3,4-thiadiazoline analogue in tumor cells

[3] Ludovica Taglieri, et al. The kinesin Eg5 inhibitor K858 induces apoptosis and reverses the malignant invasive phenotype in human glioblastoma cells

[4] Francesca De Iuliis, et al. The kinesin Eg5 inhibitor K858 induces apoptosis but also survivin-related chemoresistance in breast cancer cells

[5] Ryuichiro Nakai, et al. K858, a novel inhibitor of mitotic kinesin Eg5 and antitumor agent, induces cell death in cancer cells

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Keywords: K-858, Racemic supplier, Kinesin, inhibitors, activators


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